|Targets||Ribosomal S6 Kinase (RSK)|
|Description||FMK is a potent, highly specific and irreversible ribosomal s6 kinase (RSK) inhibitor that covalently modifies the C-terminal kinase domain of RSK. Its IC50 value is 15 nM. It could prevent the activation of the N-terminal kinase domain of RSK by the C-terminal kinase domain, but does not affect the activity of the N-terminal domain. It binds in the CTKD ATP-binding site and inhibits RSK autophosphorylation at Ser386. It induces significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells. It is used to determine the role of RSK as a direct regulator of NHE1 phosphorylation and sarcolemmal NHE activity in this cell type, in response to 1-adrenergic stimulation.|
|Appearance||White to off-white solid|
|Synonyms||1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone;RSK2 kinase inhibitor|
|Solubility||10 mM in DMSO|
|Application||FMK could prevent the activation of the N-terminal kinase domain of RSK by the C-terminal kinase domain, but does not affect the activity of the N-terminal domain. It is used to determine the role of RSK as a direct regulator of NHE1 phosphorylation and sarcolemmal NHE activity in this cell type, in response to 1-adrenergic stimulation.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Boiling Point||633.3±55.0 °C | Condition: Press: 760 Torr|
|Density||1.36±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
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